Zyvox


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linezolid

Zyvox, Zyvoxam (CA)

Pharmacologic class: Oxazolidinone

Therapeutic class: Anti-infective

Pregnancy risk category C

Action

Selectively binds to bacterial 23S ribosomal RNA of 50S subunit, preventing formation of essential component of bacterial protein synthesis. Bacteriostatic or bactericidal against gram-positive and some gram-negative bacteria.

Availability

Injection: 2 mg/ml

Powder for oral suspension: 100 mg/5 ml

Tablets: 400 mg, 600 mg

Indications and dosages

Vancomycin-resistant Enterococcus faecium infections

Adults and children ages 12 and older: 600 mg P.O. or I.V. infusion q 12 hours for 14 to 28 days

Children from birth to age 11: 10 mg/kg I.V. q 8 hours for 14 to 28 days

Nosocomial pneumonia; community-acquired pneumonia; complicated skin and skin-structure infections

Adults and children ages 12 and older: 600 mg P.O. or I.V. infusion q 12 hours for 10 to 14 days

Children from birth to age 11: 10 mg/kg P.O. or I.V. q 8 hours for 10 to 14 days

Uncomplicated skin and soft-tissue infections

Adults: 400 mg P.O. q 12 hours for 10 to 14 days

Adolescents: 600 mg P.O. or I.V. q 12 hours for 10 to 14 days

Children ages 5 to 11: 10 mg/kg P.O. or I.V. q 12 hours for 10 to 14 days

Children younger than age 5: 10 mg/kg P.O. or I.V. q 8 hours for 10 to 14 days

Contraindications

• Hypersensitivity to drug or its components

Precautions

Use cautiously in:

• hepatic dysfunction, hypertension, hyperthyroidism, pheochromocytoma, bone marrow depression, pseudomembranous colitis

• phenylketonuria (oral suspension only)

• pregnant or breastfeeding patients.

Administration

• Give oral drug with or without food.

• For I.V. injection, use single-use, ready-to-use infusion bag. Check for particulate matter before giving. Infuse over 30 minutes to 2 hours.

• For I.V. infusion, mix with dextrose 5% in water, normal saline solution, or lactated Ringer's injection.

• Flush I.V. line before and after administering, to avoid incompatibilities.

Adverse reactions

CNS: anxiety, confusion, difficulty speaking, dizziness, hallucinations, lethargy, paresthesia, light-headedness, fatigue, drowsiness, headache, seizures

GI: nausea, vomiting, diarrhea, gastritis, anorexia, dry mouth, pseudomembranous colitis

Hematologic: thrombocytopenia

Skin: rash, photosensitivity, diaphoresis

Other: fever, fungal infections

Interactions

Drug-drug. Antiplatelet drugs (such as aspirin, dipyridamole, nonsteroidal anti-inflammatory drugs): increased bleeding risk

MAO inhibitors, pseudoephedrine: increased risk of hypertension and associated adverse effects

Serotonergics: serotonin syndrome

Drug-diagnostic tests. Prothrombin time: altered

Drug-food. Tyramine-containing foods and beverages (such as beer; Chianti and certain other red wines; aged cheese; bananas; aged, cured, or spoiled meats; salted herring and other dried fish; avocado; bean curd; red plums; soy sauce; spinach; tofu, tomatoes; yeast): hypertension

Patient monitoring

• Monitor neurologic status. Institute safety measures as needed to prevent injury.

• Check I.V. site for infiltration.

Watch for bleeding and signs and symptoms of other adverse reactions (especially pseudomembranous colitis).

• Monitor CBC, coagulation studies, and culture and sensitivity tests.

Patient teaching

• Tell patient he may take with or without food, but should avoid foods containing tyramine.

Tell patient to promptly report bleeding or severe diarrhea.

• Instruct patient to minimize adverse GI effects by eating small, frequent servings of healthy food.

• Caution patient to avoid driving and other hazardous activities until he knows how drug affects concentration and alertness.

• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, and foods mentioned above.

linezolid

(li-nez-o-lid) ,

Zyvox

(trade name),

Zyvoxam

(trade name)

Classification

Therapeutic: anti infectives
Pharmacologic: oxazolidinones
Pregnancy Category: C

Indications

Treatment of:
  • Infections caused by vancomycin-resistant Enterococcus faecium,
  • Nosocomial pneumonia caused by Staphylococcus aureus (methicillin-susceptible and -resistant strains),
  • Complicated skin/skin structure infections caused by Staphylococcus aureus (methicillin-susceptible and -resistant strains), Streptococcus pyogenes or Streptococcus agalactiae (including diabetic foot infections),
  • Uncomplicated skin/skin structure infections caused by Staphylococcus aureus (methicillin-susceptible and -resistant strains), Streptococcus pyogenes,
  • Community-acquired pneumonia caused by Streptococcus pneumoniae (including multi-drug resistant strains) or Staphylococcus aureus (methicillin-susceptible strains only).

Action

Inhibits bacterial protein synthesis at the level of the 23S ribosome of the 50S subunit.

Therapeutic effects

Bactericidal action against streptococci; bacteriostatic action against enterococci and staphylococci.

Pharmacokinetics

Absorption: Rapidly and extensively (100%) absorbed following oral administration.
Distribution: Readily distributes to well-perfused tissues.
Metabolism and Excretion: 65% metabolized, mostly by the liver; 30% excreted unchanged by the kidneys.
Half-life: 6.4 hr.

Time/action profile

ROUTEONSETPEAKDURATION
POrapid1–2 hr12 hr
IVrapidend of infusion12 hr

Contraindications/Precautions

Contraindicated in: Hypersensitivity;Phenylketonuria (suspension contains aspartame);Uncontrolled HTN, pheochromocytoma, thyrotoxicosis, or concurrent use of sympathomimetic agents, vasopressors, or dopaminergic agents (↑ risk of hypertensive response);Concurrent or recent (<2 wk) use of monoamine oxidase (MAO) inhibitors (↑ risk of hypertensive response);Carcinoid syndrome or concurrent use of SSRIs, TCAs, triptans, meperidine, or buspirone (↑ risk of serotonin syndrome).
Use Cautiously in: Thrombocytopenia, concurrent use of antiplatelet agents or bleeding diathesis (platelet counts should be monitored more frequently);Diabetes (↑ risk of hypoglycemia) Obstetric: Safety not established; use only if maternal benefit outweighs potential risk to fetus; Lactation: Lactation.

Adverse Reactions/Side Effects

Cardiovascular

  • headache
  • insomnia

Ear, Eye, Nose, Throat

  • teeth discoloration
  • tongue discoloration

Gastrointestinal

  • pseudomembranous colitis (life-threatening)
  • diarrhea
  • ↑ liver enzymes
  • nausea
  • taste alteration
  • vomiting

Endocrinologic

  • hypoglycemia

Fluid and Electrolyte

  • lactic acidosis

Hematologic

  • thrombocytopenia

Neurologic

  • optic neuropathy
  • peripheral neuropathy

Interactions

Drug-Drug interaction

↑ risk of hypertensive response with MAO inhibitors, sympathomimetics (e.g., pseudoephedrine ), vasopressors (e.g., epinephrine, norepinephrine ), and dopaminergic agents (e.g., dopamine, dobutamine ); concurrent or recent use should be avoided.↑ risk of serotonin syndrome with SSRIs, TCAs, triptans, meperidine, bupropion, or buspirone ; avoid concurrent use.Rifampin, carbamazepine, phenytoin, and phenobarbital may ↓ levels.Concurrent use with oral hypoglycemics or insulin may ↑ risk of hypoglycemiaBecause of monoamine oxidase inhibitory properties, consumption of large amounts of foods or beverages containing tyramine should be avoided (↑ risk of pressor response. See ).

Route/Dosage

Vancomycin-Resistant Enterococcus faecium Infections
Oral Intravenous (Adults) 600 mg every 12 hr for 14–28 days.
Oral Intravenous (Children birth-11 yr) (in the first week of life, pre-term neonates may initially receive 10 mg/kg every 12 hr).
Pneumonia, Complicated Skin/Skin Structure Infections
Oral Intravenous (Adults) 600 mg every 12 hr for 10–14 days.
Oral Intravenous (Children birth-11 yr) 10 mg/kg every 8 hr for 10–14 days (in the first week of life, pre-term neonates may initially receive 10 mg/kg every 12 hr).
Uncomplicated Skin/Skin Structure Infections
Oral (Adults) 400 mg q 12 hr for 10–14 days.
Oral Intravenous (Children 5–11 yr) 10 mg/kg every 12 hr for 10–14 days.
Oral Intravenous (Children <5 yr) 10 mg/kg every 8 hr for 10–14 days (in the first week of life, pre-term neonates may initially receive 10 mg/kg every 12 hr).

Availability (generic available)

Oral suspension: orange: 20 mg/mL
Tablets: 600 mg
Premixed infusion: 200 mg/100 mL, 400 mg/200 mL, 600 mg/300 mL

Nursing implications

Nursing assessment

  • Assess for infection (vital signs; appearance of wound, sputum, urine, and stool; WBC) at beginning of and during therapy.
  • Obtain specimens for culture and sensitivity prior to initiating therapy. First dose may be given before receiving.
  • May cause lactic acidosis. Notify health care professional if recurrent nausea and vomiting, unexplained acidosis or low bicarbonate levels occur.
  • Monitor visual function in patients receiving linezolid for ≥3 mo or who report visual symptoms (changes in acuity or color vision, blurred vision, visual field defect) regardless of length of therapy. If optic neuropathy occurs therapy should be reconsidered.
  • Monitor bowel function. Diarrhea, abdominal cramping, fever, and bloody stools should be reported to health care professional promptly as a sign of pseudomembranous colitis. May begin up to several weeks following cessation of therapy.
  • Monitor patient taking serotonergic drugs for signs of serotonin syndrome (hyperthermia, rigidity, myoclonus, autonomic instability, mental status changes (extreme agitation progressing to delirium and coma) for two weeks (five weeks if fluoxetine was taken) or until 24 hours after the last dose of linezolid, whichever comes first.
  • Lab Test Considerations: May cause bone marrow suppression, anemia, leukopenia, pancytopenia. Monitor CBC and platelet count weekly, especially in patients at risk for increased bleeding, having pre-existing bone marrow suppression, receiving concurrent medications that may cause myelosuppression, or requiring >2 weeks of therapy. Discontinue therapy if bone marrow suppression occurs or worsens.
    • May cause ↑ AST, ALT, LDH, alkaline phosphatase and BUN.
    • May cause hypoglycemia requiring decrease in dose of antidiabetic agent or discontinuation of linezolid.

Potential Nursing Diagnoses

Risk for infection (Indications)
Diarrhea (Adverse Reactions)

Implementation

  • Dose adjustment is not necessary when switching from IV to oral dose.
  • Oral: May be administered with or without food.
    • Before using oral solution gently invert 3–5 times to mix; do not shake. Store at room temperature.
  • Intravenous Administration
  • Intermittent Infusion: Diluent: Premixed infusions are already diluted and ready to use. Solution is yellowish in color which may intensify over time without affecting its potency.Concentration: 2 mg/mL.
  • Rate: Infuse over 30–120 minutes. Flush line before and after infusion.
  • Y-Site Compatibility: acyclovir, alemtuzumab, alfentanil, allopurinol, amifostine, amikacin, aminophylline, amiodarone, amphotericin B lipid complex, amphotericin B liposome, ampicillin, ampicillin/sulbactam, anidulafungin, argatroban, atracurium, azithromycin, aztreonam, bivalirudin, bleomycin, bumetanide, buprenorphine, busulfan, butorphanol, calcium acetate, calcium chloride, calcium gluconate, carboplatin, carmustine, caspofungin, cefazolin, cefepime, cefotaxime, cefoxitin, ceftazidime, ceftriaxone, cefuroxime, chloramphenicol, ciprofloxacin, cisatracurium, cisplatin, clindamycin, cyclophosphamide, cyclosporine, cytarabine, dactinomycin, daptomycin, dexamethasone sodium phosphate, dexmedetomidine, dexrazoxane, digoxin, diltiazem, diphenhydramine, dobutamine, docetaxel, dolasetron, dopamine, doripenem, doxorubicin, doxorubicin liposome, doxycycline, droperidol, enalaprilat, ephedrine, epinephrine, epirubicin, eptifibatide, ertapenem, esmolol, etoposide, etoposide phosphate, famotidine, fenoldopam, fentanyl, fluconazole, fludarabine, fluorouracil, foscarnet, fosphenytoin, furosemide, ganciclovir, gemcitabine, gentamicin, glycopyrrolate, granisetron, haloperidol, heparin, hydralazine, hydrocortisone, hydromorphone, idarubicin, ifosfamide, imipenem/cilastatin, insulin, irinotecan, isoproterenol, ketorolac, labetalol, leucovorin, levofloxacin, lidocaine, lorazepam, magnesium sulfate, mannitol, mechlorethamine, melphalan, meperidine, meropenem, mesna, methotrexate, methyldopate, methylprednisolone, metoclopramide, metoprolol, metronidazole, midazolam, milrinone, mitoxantrone, morphine, mycophenolate, nafcillin, nalbuphine, naloxone, nesiritide, nicardipine, nitroglycerin, nitroprusside, norepinephrine, octreotide, ondansetron, oxaliplatin, oxytocin, paclitaxel, palonosetron, pamidronate, pancuronium, pemetrexed, pentazocine, pentobarbital, phenobarbital, phentolamine, phenylephrine, piperacillin/tazobactam, potassium acetate, potassium chloride, potassium phosphates, procainamide, prochlorperazine, promethazine, propranolol, quinupristin/dalfopristin, ranitidine, remifentanil, rocuronium, sodium acetate, sodium bicarbonate, sodium phosphates, streptozocin, succinylcholine, sufentanil, tacrolimus, teniposide, theophylline, thiotepa, ticarcillin/clavulanate, tigecycline, tirofiban, tobramycin, trimethoprim/sulfamethoxazole, vancomycin, vasopressin, vecuronium, verapamil, vinblastine, vincristine, vinorelbine, voriconazole, zidovudine, zoledronic acid
  • Y-Site Incompatibility: amphotericin B colloidal, chlorpromazine, dantrolene, diazepam, pantoprazole, pentamidine, phenytoin, thiopental

Patient/Family Teaching

  • Advise patients taking oral linezolid to take as directed, for full course of therapy, even if feeling better. Take missed doses as soon as remembered unless almost time for next dose; do not double dose.
  • Instruct patient to avoid large quantities of foods or beverages containing tyramine (See ). May cause hypertensive response.
  • Instruct patient to notify health care professional if patient has a history of hypertension or seizures.
  • Advise patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult with health care professional before taking other medications, especially cold remedies, decongestants, or antidepressants.
  • Instruct patient to notify health care professional if changes in vision occur or immediately if diarrhea, abdominal cramping, fever, or bloody stools occur and not to treat with antidiarrheals without consulting health care professionals.
  • Advise patient to notify health care professional if no improvement is seen in a few days.

Evaluation/Desired Outcomes

  • Resolution of signs and symptoms of infection. Length of time for complete resolution depends on organism and site of infection.

Zyvox

Linezolid Infectious disease An oxazolidinone class antibiotic active against gram-positive bacteria Indications Skin and soft-tissue infections, community-acquired and hospital-acquired pneumonia, gram-positive–eg, MRSA, VRE bacteremia. See Methicillin-resistant Staphylococcus aureus, Vancomycin-resistant enterococci.
References in periodicals archive ?
Caffrey's research was partially funded by Pfizer, which markets linezolid as Zyvox.
The three major drugs in this area all have side effect issues: Zyvox has been reported to cause myelosuppression, hematological adverse events, and optic neuropathy, whereas Invanz and Zosyn are associated with hypersensitivity reactions, and Invanz has the potential to cause seizures.
Los antibioticos que se pueden seleccionar para ser utilizado son la vancomicina, linezolid (Zyvox), carbapenemicos, penicilinas antipseudomonica, las cefalosporinas de cuarta generacion, y otros menos frecuentes como la daptomicina (Cubicin), quinupristina/dalfopristina (Synercid), colistina y la tigeciclina (Tygacil).
While future sales for an early-stage molecule are difficult to predict, two of the top-selling branded antibiotics, Pfizer Inc.'s (New York) Zyvox and Cubicin, from Cubist Pharmaceuticals Inc.
A detailed analysis of a 2002 case in Michigan showed that the identified VRSA organism was susceptible to quinupristin-dalfopristin (Synercid) and to linezolid (Zyvox) (Chang et al., 2003), however the isolated organisms in the other cases are likely from different strains and susceptibilities may be different.
A relatively new drug, Zyvox, could be used for her, and even its oral form achieved great results in kids.
The companies had illegally promoted several drugs for off-label use, including Bextra, an anti-inflammatory; Geodon, an anti-psychotic; Zyvox, an antibiotic; and Lyrica, an anti-epileptic drug.
Pfizer's $1 billion civil penalty is to resolve civil allegations of illegally promoting three other drugs in addition to Bextra drugs--Geodon, an anti-psychotic drug; Zyvox, an antibiotic; and Lyrica, an anti-epileptic drug.
Radezolid is a novel oxazolidinone that was discovered using Rib-X's proprietary discovery process and was designed to expand the bacterial spectrum and improve the utility of this class of antibiotics relative to the only other oxazolidinone marketed in the world, Zyvox (linezolid).
Between April and June of this year, 12 patients in an intensive care unit at the Hospital Clinico San Carlos in Madrid were identified as having methicillin-resistant Staphylococcus aureus (MRSA) that was also resistant to linezolid (Zyvox).
Effective antibiotics include sulfamethoxazole and trimethoprim (Bactrim), doxycycline (Doryx, Monodox), and a newer drug, linezolid (Zyvox).
In addition to Chantix, Pfizer's pharmaceutical product offerings include Lipitor, a blockbuster drug that helps to lower blood cholesterol, Norvasc for the management of high blood pressure, Caduet for cardiovascular issues, Lyrica for neuropathic pain, Aricept for Alzheimer's disease, Zoloft for the treatment of depression and anxiety, Celebrex for arthritis pain, inflammation and acute pain, Zyvox for bacterial infections, Selzentry/Celsentri for some forms of HIV, Viagra for erectile dysfunction, and Zyrtec for allergies and hives, among others.